Rivaroxaban-containing composition and preparation method thereof

A technology of rivaroxaban and composition, which is applied in the field of compositions containing rivaroxaban, can solve the problems of cumbersome process, high energy consumption, and drug degradation reaction, and achieve the effect of wide application and increased dissolution

Active Publication Date: 2015-10-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the dry granulation and direct compression process, this method has cumbersome process

Method used

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  • Rivaroxaban-containing composition and preparation method thereof
  • Rivaroxaban-containing composition and preparation method thereof
  • Rivaroxaban-containing composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example

[0028] Determination and comparison implementation 1 disintegration: about 6.5 minutes;

[0029] Dissolution: Dissolution conditions: USP paddle method, 900 ml sodium acetate buffer pH 4.5 containing 0.5% sodium dodecyl sulfate, rotating speed 75 rpm). Samples were taken at 15, 30, 45 and 60 min respectively, filtered, and the subsequent filtrate was measured by HPLC, and the cumulative dissolution percentage was calculated.

[0030] Dissolution Results

[0031]

Example Embodiment

[0050] Example 1

[0051] Composition of Rivaroxaban / per tablet:

[0052]

[0053] Among them, rivaroxaban is the micronized crystal form I, and the particle size distribution is X 50 =3.5μm, X 90 =7.6μm

[0054] Preparation Process:

[0055] Using methods known in the pharmaceutical industry, mix rivaroxaban with β-cyclodextrin, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate and micropowder silica gel into the hopper of a dry granulator In the process, the drug-containing flakes are rolled with a pressure of 5-7Mpa, and then pulverized with a 30-mesh sieve to prepare granules. The obtained granules are mixed with magnesium stearate and then compressed into tablets with a diameter of 6 mm and a hardness of 60-90N. The obtained tablet is coated with a coating material consisting of iron oxide, hydroxypropyl methylcellulose and polyethylene glycol.

Example Embodiment

[0056] Example 2

[0057] Composition of Rivaroxaban / per capsule:

[0058]

[0059] Among them, rivaroxaban is the micronized crystal form I, and the particle size distribution is X 50 =4.8μm, X 90 =9.2μm

[0060] Preparation Process:

[0061] Using a method known in the pharmaceutical industry, rivaroxaban was mixed with α-cyclodextrin, micropowder silica gel and sodium lauryl sulfate, and was placed in a No. 1 capsule by a capsule filling machine.

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Abstract

The invention discloses a rivaroxaban-containing composition and a preparation method thereof. The composition contains rivaroxaban and cyclodextrin with a weight ratio of (1: 1) to (1: 20). The composition disclosed by the invention is wide in process application range, and capable of improving rivaroxaban dissolution and guaranteeing no influences of a preparation process on the bioavailability.

Description

technical field [0001] The invention relates to a composition containing rivaroxaban and a preparation method thereof. Background technique [0002] Rivaroxaban (Rivaroxaban), the chemical name is 5-chloro-nitrogen-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1, 3-oxazolidin-5-yl}-2-thiophene-carboxamide, its structural formula is as shown in formula (I): [0003] [0004] Rivaroxaban is the world's first oral direct factor Xa inhibitor, which can highly selectively and competitively inhibit free and bound Xa coagulation factor, interrupt the intrinsic and extrinsic pathways of blood coagulation, thereby inhibiting the thrombin generation and thrombosis. [0005] Rivaroxaban is a highly hydrophobic and poorly soluble drug with a low solubility in water (about 7 mg / L). Appropriate solubilization techniques must be used to achieve the desired therapeutic effect. Bayer applied for protection of a wet granulation process of rivaroxaban and its composition (method for pre...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/5377A61P7/02A61P9/10A61P9/14
Inventor 陶涛柴旭煜谢双赵雁陈中亚印玺璟
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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